SOLID DISPERSION CONTAINING LEFLUNOMIDE AND PREPARATION METHOD THEREOF

摘要

Solid dispersion containing leflunomide having anti-rheumatic effects is provided to increase bioavailability of leflunomide by improving its in vivo solubility and release rate by using hydroxypropylmethylcellulose as resin. A method for preparing the solid dispersion containing leflunomide comprises the steps of: solubilizing leflunomide and hydroxypropylmethylcellulose 2910 in mixed solvent of polar solvent selected from ethanol, propanol and isopropanol and nonpolar solvent selected from trichloromethane, dichloromethane and chloroform; adding nonpolar surfactant such as polysorbate(tween) into the mixture and mixing them; and spray-drying the mixture with a spray-dryer. A pharmaceutical composition comprises the solid dispersion containing leflunomide, and is formulated as tablet, capsule or coated tablet.